sensory system agents


Summary: Drugs that act on neuronal sensory receptors resulting in an increase, decrease, or modification of afferent nerve activity. (From Smith and Reynard, Textbook of Pharmacology, 1991, p367)

Top Publications

  1. England J, Wagner T, Kern K, Roth Daniek A, Sell A. The capsaicin 8% patch for peripheral neuropathic pain. Br J Nurs. 2011;20:926-31 pubmed
    ..The observations and learning that the authors have gained from their clinical experience with the capsaicin 8% patch will help others to maximize the benefit gained with this novel treatment option. ..
  2. Sikand P, Shimada S, Green B, LaMotte R. Sensory responses to injection and punctate application of capsaicin and histamine to the skin. Pain. 2011;152:2485-94 pubmed publisher
  3. Papoiu A, Yosipovitch G. Topical capsaicin. The fire of a 'hot' medicine is reignited. Expert Opin Pharmacother. 2010;11:1359-71 pubmed publisher
    ..Capsaicin has been proven a truly exciting molecule and remains a valuable drug for alleviating pain and itch, widely surpassing its role as a simple spicy ingredient. ..
  4. Wallace M, Schulteis G, Atkinson J, Wolfson T, Lazzaretto D, Bentley H, et al. Dose-dependent effects of smoked cannabis on capsaicin-induced pain and hyperalgesia in healthy volunteers. Anesthesiology. 2007;107:785-96 pubmed
    ..There was no significant difference in performance on the neuropsychological tests. This study suggests that there is a window of modest analgesia for smoked cannabis, with lower doses decreasing pain and higher doses increasing pain. ..
  5. Backonja M, Malan T, Vanhove G, Tobias J. NGX-4010, a high-concentration capsaicin patch, for the treatment of postherpetic neuralgia: a randomized, double-blind, controlled study with an open-label extension. Pain Med. 2010;11:600-8 pubmed publisher
    ..No patients discontinued the study due to an adverse event. NGX-4010 is a promising topical treatment for PHN patients, which appears to be tolerable, generally safe, and effective. ..
  6. Noma N, Tsuboi Y, Kondo M, Matsumoto M, Sessle B, Kitagawa J, et al. Organization of pERK-immunoreactive cells in trigeminal spinal nucleus caudalis and upper cervical cord following capsaicin injection into oral and craniofacial regions in rats. J Comp Neurol. 2008;507:1428-40 pubmed publisher
  7. Webster L, Tark M, Rauck R, Tobias J, Vanhove G. Effect of duration of postherpetic neuralgia on efficacy analyses in a multicenter, randomized, controlled study of NGX-4010, an 8% capsaicin patch evaluated for the treatment of postherpetic neuralgia. BMC Neurol. 2010;10:92 pubmed publisher
    ..nct00068081. ..
  8. Anand U, Otto W, Bountra C, Chessell I, Sinisi M, Birch R, et al. Cytosine arabinoside affects the heat and capsaicin receptor TRPV1 localisation and sensitivity in human sensory neurons. J Neurooncol. 2008;89:1-7 pubmed publisher
  9. Peters J, McDougall S, Fawley J, Smith S, Andresen M. Primary afferent activation of thermosensitive TRPV1 triggers asynchronous glutamate release at central neurons. Neuron. 2010;65:657-69 pubmed publisher
    ..This activity-dependent TPRV1-mediated facilitation is a form of synaptic plasticity that brings a unique central integrative feature to the CNS and autonomic regulation. ..

More Information


  1. McCormack P. Capsaicin dermal patch: in non-diabetic peripheral neuropathic pain. Drugs. 2010;70:1831-42 pubmed publisher
    ..Capsaicin dermal patch was generally well tolerated in clinical trials. The most common adverse events were transient, mostly mild to moderate, application-site reactions. ..
  2. Kennedy W, Vanhove G, Lu S, Tobias J, Bley K, Walk D, et al. A randomized, controlled, open-label study of the long-term effects of NGX-4010, a high-concentration capsaicin patch, on epidermal nerve fiber density and sensory function in healthy volunteers. J Pain. 2010;11:579-87 pubmed publisher
    ..This article evaluates the effect of a single 60-minute NGX-4010 application on ENF density and QST in healthy volunteers followed for 24 weeks. The results help predict the long-term safety of NGX-4010 applications in patients. ..
  3. Aizawa N, Igawa Y, Andersson K, Iijima K, Nishizawa O, Wyndaele J. Effects of intravesical instillation of ATP on rat bladder primary afferent activity and its relationship with capsaicin-sensitivity. Neurourol Urodyn. 2011;30:163-8 pubmed publisher
    ..The activation of the bladder afferents induced by intravesical application of ATP is mediated mainly through Cap-insensitive C-fibers. ..
  4. Backonja M, Wallace M, Blonsky E, Cutler B, Malan P, Rauck R, et al. NGX-4010, a high-concentration capsaicin patch, for the treatment of postherpetic neuralgia: a randomised, double-blind study. Lancet Neurol. 2008;7:1106-12 pubmed publisher
    ..No adverse events were associated with treatment except for local reactions at the site of application and those related to treatment-associated pain. ..
  5. Edelsberg J, Lord C, Oster G. Systematic review and meta-analysis of efficacy, safety, and tolerability data from randomized controlled trials of drugs used to treat postherpetic neuralgia. Ann Pharmacother. 2011;45:1483-90 pubmed publisher
  6. Just T, Steiner S, Pau H. Oral pain perception and taste in burning mouth syndrome. J Oral Pathol Med. 2010;39:22-7 pubmed publisher
    ..Both pain-related and gustatory sensitivies of the tongue are found to be decreased in BMS. ..
  7. Yang X, Gong H, Liu Z, Liu H, Wang H, Li Z. Similar and different effects of capsaicin and resiniferatoxin on substance P release and transient receptor potential vanilloid type 1 expression of cultured rat dorsal root ganglion neurons. Methods Find Exp Clin Pharmacol. 2010;32:3-11 pubmed publisher
    ..The efficacy and therapeutic potential of the reversible action of RTX are more applicable as strategies for pain or neurogenic inflammation therapy. ..
  8. Wu C, Gavva N, Brennan T. Effect of AMG0347, a transient receptor potential type V1 receptor antagonist, and morphine on pain behavior after plantar incision. Anesthesiology. 2008;108:1100-8 pubmed publisher
    ..AMG0347 only decreased heat hyperalgesia after plantar incision even though both peripheral and central TRPV1 receptors were blocked. The smallest doses of morphine affected guarding pain and heat responses. ..
  9. Knotkova H, Pappagallo M, Szallasi A. Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival?. Clin J Pain. 2008;24:142-54 pubmed publisher
  10. Malin S, Christianson J, Bielefeldt K, Davis B. TPRV1 expression defines functionally distinct pelvic colon afferents. J Neurosci. 2009;29:743-52 pubmed publisher
    ..These results suggest a unique functional role of TRPV1-positive colon afferents that could be exploited to design specific therapies for visceral hypersensitivity. ..
  11. Liu Z, Li Z. Regulation of galanin and galanin receptor 2 expression by capsaicin in primary cultured dorsal root ganglion neurons. In Vitro Cell Dev Biol Anim. 2008;44:379-84 pubmed publisher
    ..The possible significance of the neurotransmission of nociceptive information involved in galanin or GalR2 expression caused by capsaicin is still to be clarified. ..
  12. Kosuwon W, Sirichatiwapee W, Wisanuyotin T, Jeeravipoolvarn P, Laupattarakasem W. Efficacy of symptomatic control of knee osteoarthritis with 0.0125% of capsaicin versus placebo. J Med Assoc Thai. 2010;93:1188-95 pubmed
    ..The burning sensation reported by patients in the capsaicin group was less disturbing than in previous studies and none of the present patients withdrew for this reason. ..
  13. Calzetta L, Spina D, Cazzola M, Page C, Facciolo F, Rendina E, et al. Pharmacological characterization of adenosine receptors on isolated human bronchi. Am J Respir Cell Mol Biol. 2011;45:1222-31 pubmed publisher
    ..05). This study provides evidence for a role for adenosine A(1) receptors in eliciting human airway smooth muscle constriction, which, in part, is mediated by the action of capsaicin sensitive sensory nerves. ..
  14. Lin A, Lin C, Tung H, Chary N. Potential for biodegradation and sorption of acetaminophen, caffeine, propranolol and acebutolol in lab-scale aqueous environments. J Hazard Mater. 2010;183:242-50 pubmed publisher
    ..These results suggest that mechanisms other than hydrophobic interactions played an important role in the sorption process...
  15. Patil M, Jeske N, Akopian A. Transient receptor potential V1 regulates activation and modulation of transient receptor potential A1 by Ca2+. Neuroscience. 2010;171:1109-19 pubmed publisher
    ..In summary, activation of TRPA1 by [Ca(2+)](e) and [Ca(2+)](i) is controlled by the TRPV1 channel, and characteristics of I(MO) depend on Ca(2+) permeability of the TRPV1 channel. ..
  16. Zhou Y, Sun B, Li Q, Luo P, Dong L, Rong W. Sensitivity of bronchopulmonary receptors to cold and heat mediated by transient receptor potential cation channel subtypes in an ex vivo rat lung preparation. Respir Physiol Neurobiol. 2011;177:327-32 pubmed publisher
    ..Moreover, cold-evoked responses was unaffected by TRPA1 antagonist HC-03001. Our observations suggest that TRPV1 and TRPM8 are involved in transducing heat and cold in the lower respiratory tract, respectively. ..
  17. Liu Z, Zhang F, Liu H, Yang X, Wang H, Li Z. Co-administration of nerve growth factor and butyrate regulates vanilloid receptor 1 and substance P levels in cultures of rat dorsal root ganglion neurons. Acta Physiol Hung. 2009;96:231-41 pubmed publisher
    ..The mechanisms of the effects of co-administration of NGF and butyrate should be clarified by further study. ..
  18. Fehrenbacher J, Sun X, Locke E, Henry M, Hargreaves K. Capsaicin-evoked iCGRP release from human dental pulp: a model system for the study of peripheral neuropeptide secretion in normal healthy tissue. Pain. 2009;144:253-61 pubmed publisher
    ..These results indicate that the release of iCGRP from human dental pulp provides a novel tool to determine the effects of pharmacological compounds on human nociceptor sensitivity. ..
  19. Zhai X, Lu Y. Food-drug interactions: effect of capsaicin on the pharmacokinetics of galantamine in rats. Xenobiotica. 2012;42:1151-5 pubmed publisher
    ..05-fold by pretreatment with CAP (p < 0.05). These results demonstrate that the chronic ingestion of high doses of CAP will decrease the bioavailability of galantamine to a significant extent in rats. ..
  20. Starowicz K, Maione S, Cristino L, Palazzo E, Marabese I, Rossi F, et al. Tonic endovanilloid facilitation of glutamate release in brainstem descending antinociceptive pathways. J Neurosci. 2007;27:13739-49 pubmed
    ..The results obtained with the TRPV1 antagonist alone suggest that this pathway is tonically activated by endovanilloids. ..
  21. Leung F. Capsaicin-sensitive intestinal mucosal afferent mechanism and body fat distribution. Life Sci. 2008;83:1-5 pubmed publisher
    ..The hypothesis that the intestinal mucosal afferent mechanism is a plausible therapeutic target for abating visceral obesity deserves to be further evaluated. ..
  22. Rosenkranz M, Davidson R, MacCoon D, Sheridan J, Kalin N, Lutz A. A comparison of mindfulness-based stress reduction and an active control in modulation of neurogenic inflammation. Brain Behav Immun. 2013;27:174-84 pubmed publisher
    ..Moreover, mindfulness practice, in particular, may be more efficacious in symptom relief than the well-being promoting activities cultivated in the HEP program...
  23. Kim H, Cui L, Kim J, Kim S. Transient receptor potential vanilloid type 1 receptor regulates glutamatergic synaptic inputs to the spinothalamic tract neurons of the spinal cord deep dorsal horn. Neuroscience. 2009;160:508-16 pubmed publisher
    ..These data suggest that activation of TRPV1 potentiates the glutamate release from excitatory terminals of primary afferent fibers and subsequently increases the neural activity of STT neurons of the rat spinal cord deep dorsal horn. ..
  24. Toth B, Géczy T, Griger Z, Dózsa A, Seltmann H, Kovacs L, et al. Transient receptor potential vanilloid-1 signaling as a regulator of human sebocyte biology. J Invest Dermatol. 2009;129:329-39 pubmed publisher
  25. Samuelsen C, Gardner M, Fontanini A. Effects of cue-triggered expectation on cortical processing of taste. Neuron. 2012;74:410-22 pubmed publisher
    ..Altogether, these data provide a model for how cue-triggered expectation changes the state of sensory cortices to achieve rapid processing of natural stimuli. ..
  26. Bortolotti M, Porta S. Effect of red pepper on symptoms of irritable bowel syndrome: preliminary study. Dig Dis Sci. 2011;56:3288-95 pubmed publisher
  27. Picazo Juárez G, Romero Suarez S, Nieto Posadas A, Llorente I, Jara Oseguera A, Briggs M, et al. Identification of a binding motif in the S5 helix that confers cholesterol sensitivity to the TRPV1 ion channel. J Biol Chem. 2011;286:24966-76 pubmed publisher
    ..These data suggest that there is a cholesterol-binding site in TRPV1 and that the functions of TRPV1 depend on the genetic variant and membrane cholesterol content. ..
  28. Sculptoreanu A, Aura Kullmann F, de Groat W. Neurokinin 2 receptor-mediated activation of protein kinase C modulates capsaicin responses in DRG neurons from adult rats. Eur J Neurosci. 2008;27:3171-81 pubmed publisher
    ..Thus, activation of NK2 autoreceptors by NKs released from the peripheral afferent terminals or by mast cells during inflammatory responses may be a mechanism that sensitizes TRPV1 channels and enhances afferent excitability. ..
  29. Ho C, Tan C, Tsai H, Kou Y. Ozone-induced nasal hyperresponsiveness to tachykinins in guinea pigs. Am J Rhinol. 2008;22:463-7 pubmed publisher
    ..It is possibly mediated through the suppressive action of ozone on the tachykinin degradation. ..
  30. Han L, Ma C, Liu Q, Weng H, Cui Y, Tang Z, et al. A subpopulation of nociceptors specifically linked to itch. Nat Neurosci. 2013;16:174-82 pubmed publisher
    ..These data suggest that MrgprA3 defines a specific subpopulation of DRG neurons mediating itch. Our study opens new avenues for studying itch and developing anti-pruritic therapies. ..
  31. Gris P, Cheng P, Pierson J, Maixner W, Diatchenko L. Molecular assays for characterization of alternatively spliced isoforms of the u opioid receptor (MOR). Methods Mol Biol. 2010;617:421-35 pubmed publisher
    ..In this review, we describe the methodologies used to assay key mediators of MOR activation including cellular assays for cAMP, free Ca(2+), and NO, all of which have been implicated in the pharmacological effects of MOR agonists. ..
  32. Benedetti M, Merino R, Kusuda R, Ravanelli M, Cadetti F, Dos Santos P, et al. Plasma corticosterone levels in mouse models of pain. Eur J Pain. 2012;16:803-15 pubmed publisher
    ..Therefore, HPA-axis activation represents an important variable to be considered when designing experimental assays of persistent pain as well as for interpretation of data. ..
  33. Changani K, Hotee S, Campbell S, Pindoria K, Dinnewell L, Saklatvala P, et al. Effect of the TRPV1 antagonist SB-705498 on the nasal parasympathetic reflex response in the ovalbumin sensitized guinea pig. Br J Pharmacol. 2013;169:580-9 pubmed publisher
    ..We propose that TRPV1 is pivotal in initiating symptoms of rhinitis. ..
  34. Iannetti G, Baumgartner U, Tracey I, Treede R, Magerl W. Pinprick-evoked brain potentials: a novel tool to assess central sensitization of nociceptive pathways in humans. J Neurophysiol. 2013;110:1107-16 pubmed publisher
  35. Rofes L, Arreola V, Martin A, Clave P. Natural capsaicinoids improve swallow response in older patients with oropharyngeal dysphagia. Gut. 2013;62:1280-7 pubmed publisher
    ..Stimulation of TRPV1 by capsaicinoids strongly improved safety and efficacy of swallow and shortened the swallow response in older patients with OD. Stimulation of TRPV1 might become a pharmacologic strategy to treat OD. ..
  36. Kadekawa K, Majima T, Shimizu T, Wada N, de Groat W, Kanai A, et al. The role of capsaicin-sensitive C-fiber afferent pathways in the control of micturition in spinal-intact and spinal cord-injured mice. Am J Physiol Renal Physiol. 2017;313:F796-F804 pubmed publisher
  37. Burness C, McCormack P. Capsaicin 8 % Patch: A Review in Peripheral Neuropathic Pain. Drugs. 2016;76:123-34 pubmed publisher
    ..The capsaicin 8 % patch was associated with expected, transient, capsaicin-related application-site adverse events such as erythema and pain. ..
  38. Bhaskaran M, Smith B. Effects of TRPV1 activation on synaptic excitation in the dentate gyrus of a mouse model of temporal lobe epilepsy. Exp Neurol. 2010;223:529-36 pubmed publisher
  39. Bhashyam A, Mogayzel P, Cleary J, Undem B, Kollarik M, Fox J, et al. Vagal control of mucociliary clearance in murine lungs: a study in a chronic preparation. Auton Neurosci. 2010;154:74-8 pubmed publisher
  40. Ohta T, Imagawa T, Ito S. Novel gating and sensitizing mechanism of capsaicin receptor (TRPV1): tonic inhibitory regulation of extracellular sodium through the external protonation sites on TRPV1. J Biol Chem. 2008;283:9377-87 pubmed publisher
  41. Wang H, Pan Y, Wang W, Gao L, Zimmerman M, Zucker I, et al. Exercise training prevents the exaggerated exercise pressor reflex in rats with chronic heart failure. J Appl Physiol (1985). 2010;108:1365-75 pubmed publisher
    ..These findings suggest a potential therapeutic role for ExT in minimizing arterial pressure and sympathetic outflow following activation of the EPR in the CHF state. ..
  42. Gad M, Pedersen A, Kristensen N, Fernandez C, Claesson M. Blockage of the neurokinin 1 receptor and capsaicin-induced ablation of the enteric afferent nerves protect SCID mice against T-cell-induced chronic colitis. Inflamm Bowel Dis. 2009;15:1174-82 pubmed publisher
    ..Our data demonstrate the importance of an intact enteric afferent nerve system and NK-1 signaling in mucosal inflammation and may suggest new treatment modalities for patients suffering from inflammatory bowel disease. ..
  43. Derry S, Moore R. Topical capsaicin (low concentration) for chronic neuropathic pain in adults. Cochrane Database Syst Rev. 2012;:CD010111 pubmed publisher
    ..Local skin irritation, which was often mild and transient but may lead to withdrawal, was common. Systemic adverse effects were rare. ..
  44. Chidiac J, Al Asmar B, Rifai K, Jabbur S, Saade N. Inflammatory mediators released following application of irritants on the rat injured incisors. The effect of treatment with anti-inflammatory drugs. Cytokine. 2009;46:194-200 pubmed publisher
    ..Our results confirm the validity of the tooth perfusion technique and demonstrate that the efficacy of treatment with anti-inflammatory drugs depends on the type of inflammation. ..
  45. Dicpinigaitis P, Gayle Y, Solomon G, Gilbert R. Inhibition of cough-reflex sensitivity by benzonatate and guaifenesin in acute viral cough. Respir Med. 2009;103:902-6 pubmed publisher
    ..008). The mechanism by which the combination of B+G causes a potentiation of antitussive effect remains to be elucidated. Our results suggest that B+G may be an effective therapy for acute cough due to the common cold (URI). ..
  46. Musella A, De Chiara V, Rossi S, Prosperetti C, Bernardi G, Maccarrone M, et al. TRPV1 channels facilitate glutamate transmission in the striatum. Mol Cell Neurosci. 2009;40:89-97 pubmed publisher
    ..TRPV1-mediated regulation of excitatory transmission in the striatum might be important for the final output to other basal ganglia structures, and might play a role in several physiological and pathological processes. ..
  47. Zagorodnyuk V, Gibbins I, Costa M, Brookes S, Gregory S. Properties of the major classes of mechanoreceptors in the guinea pig bladder. J Physiol. 2007;585:147-63 pubmed
    ..At least four functional classes of bladder mechanoreceptors can be readily distinguished by different mechanisms of activation and are likely to transmit different types of information to the central nervous system. ..
  48. Rawls S, Gomez T, Ding Z, Raffa R. Differential behavioral effect of the TRPM8/TRPA1 channel agonist icilin (AG-3-5). Eur J Pharmacol. 2007;575:103-4 pubmed
    ..This is the first demonstration of a TRPM8/TRPA1 channel subtype agonist-induced differential pharmacological effect in invertebrates and provides a novel sensitive, quantifiable end-point for studying TRP channel pharmacology. ..
  49. Chen Y, Lu M, Huang H, Ma M. Mechanosensitive transient receptor potential vanilloid type 1 channels contribute to vascular remodeling of rat fistula veins. J Vasc Surg. 2010;52:1310-20 pubmed publisher
  50. Srbely J, Dickey J, Bent L, Lee D, Lowerison M. Capsaicin-induced central sensitization evokes segmental increases in trigger point sensitivity in humans. J Pain. 2010;11:636-43 pubmed publisher
    ..Elucidating the role of central sensitization in the pathophysiology of trigger points is fundamental to developing optimal strategies in the management of myofascial pain syndrome. ..
  51. Zhao H, Sprunger L, Simasko S. Expression of transient receptor potential channels and two-pore potassium channels in subtypes of vagal afferent neurons in rat. Am J Physiol Gastrointest Liver Physiol. 2010;298:G212-21 pubmed publisher
  52. Kóbor I, Gál V, Vidnyanszky Z. Attentional modulation of perceived pain intensity in capsaicin-induced secondary hyperalgesia. Exp Brain Res. 2009;195:467-72 pubmed publisher
    ..Our findings, showing no interaction between capsaicin treatment and attentional modulation suggest that capsaicin-induced secondary hyperalgesia and attention might affect mechanical pain through independent mechanisms. ..
  53. Mou J, Paillard F, Turnbull B, Trudeau J, Stoker M, Katz N. Efficacy of Qutenza® (capsaicin) 8% patch for neuropathic pain: a meta-analysis of the Qutenza Clinical Trials Database. Pain. 2013;154:1632-9 pubmed publisher
    ..These results confirm that Qutenza is effective for the treatment of both PHN and HIV-AN compared to low-dose control patch. ..